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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1994-2-14
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pubmed:abstractText |
GYKI 52466 and related 2,3-benzodiazepines are highly selective antagonists of AMPA-evoked responses in rat CNS. However, these compounds do not compete with [3H]AMPA binding and their site of action remains unclear. Here we show that [3H]GYKI 53405 binds specifically to Xenopus brain membranes with KD and Bmax values of 4.5 microM and 35 pmol mg-1 protein respectively. Binding is increased in the presence of Mg2+ and is unaffected by AMPA or kainate. This is the first report of the binding of a GYKI 52466-related radioligand to any tissue and these results provide an initial step towards the characterization of novel recognition sites which are of considerable therapeutic potential.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
0959-4965
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
25
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pubmed:volume |
5
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
93-4
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pubmed:dateRevised |
2009-9-29
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pubmed:meshHeading |
pubmed-meshheading:7506593-Animals,
pubmed-meshheading:7506593-Benzodiazepines,
pubmed-meshheading:7506593-Brain,
pubmed-meshheading:7506593-Cell Membrane,
pubmed-meshheading:7506593-Central Nervous System,
pubmed-meshheading:7506593-Kinetics,
pubmed-meshheading:7506593-Radioligand Assay,
pubmed-meshheading:7506593-Receptors, AMPA,
pubmed-meshheading:7506593-Tritium,
pubmed-meshheading:7506593-Xenopus,
pubmed-meshheading:7506593-alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid
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pubmed:year |
1993
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pubmed:articleTitle |
Binding of the AMPA receptor antagonist [3H]GYKI 53405 to Xenopus brain membranes.
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pubmed:affiliation |
Department of Pharmacology, Medical School, University of Birmingham, Edgbaston, UK.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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